Assay Detail
Binding
CHEMBL1949346
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Citalopram from SERT in rat cerebral cortex homogenates after 1 hr by liquid scintillation counter
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.33 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485540 | — | — | 1 | 7.48 |
| CHEMBL485541 | — | — | 1 | 7.30 |
| CHEMBL485542 | — | — | 1 | 7.12 |
| CHEMBL520024 | — | — | 1 | 7.10 |
| CHEMBL483176 | — | — | 1 | 7.02 |
| CHEMBL299638 | — | — | 1 | 6.95 |
| CHEMBL297702 | — | — | 1 | 6.83 |
| CHEMBL1945686 | — | — | 1 | 6.77 |
| CHEMBL1945475 | — | — | 1 | 6.57 |
| CHEMBL1945682 | — | — | 1 | 6.21 |
| CHEMBL1945681 | — | — | 1 | 6.09 |
| CHEMBL1945678 | — | — | 1 | 6.04 |
| CHEMBL1945679 | — | — | 1 | 5.87 |
| CHEMBL1945684 | — | — | 1 | 5.55 |
| CHEMBL1945683 | — | — | 1 | 5.38 |
| CHEMBL1945685 | — | — | 1 | 4.73 |
| CHEMBL1945680 | — | — | 1 | 4.59 |
| CHEMBL41140 | 6-NITROQUIPAZINE | — | 1 | - |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485540 | — | IC50 | = | 33.4 | nM | 7.48 |
| CHEMBL485541 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL485542 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL520024 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL483176 | — | IC50 | = | 95.5 | nM | 7.02 |
| CHEMBL299638 | — | IC50 | = | 111.6 | nM | 6.95 |
| CHEMBL297702 | — | IC50 | = | 146.4 | nM | 6.83 |
| CHEMBL1945686 | — | IC50 | = | 170.7 | nM | 6.77 |
| CHEMBL1945475 | — | IC50 | = | 267.8 | nM | 6.57 |
| CHEMBL1945682 | — | IC50 | = | 616.3 | nM | 6.21 |
| CHEMBL1945681 | — | IC50 | = | 806.8 | nM | 6.09 |
| CHEMBL1945678 | — | IC50 | = | 921.1 | nM | 6.04 |
| CHEMBL1945679 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL1945684 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1945683 | — | IC50 | = | 4130.0 | nM | 5.38 |
| CHEMBL1945685 | — | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL1945680 | — | IC50 | = | 25900.0 | nM | 4.59 |
| CHEMBL41140 | 6-NITROQUIPAZINE | IC50 | - | — | - | |
| CHEMBL18772 | QUIPAZINE | IC50 | - | — | - |